Design and Synthesis of New Biarylhydrazides Possessing an Azido Pharmacophore as Selective COX-2 Inhibitors

Document Type : Original Article

Abstract

A group of 1,3-biarylhydrazide derivatives possessing a COX-2 azido pharmacophore at the Para- position of the C-1 phenyl ring in conjunction with a N-3 phenyl or substituted-phenyl ring (4-F,4-Cl,4-OMe) were designed and synthesized based on nucleophilic substitution reaction. A molecular modelling study of these compounds showed that the designed molecules were well bound with the active site of COX-2 enzyme and the N3 pharmacophore was well oriented into the COX-2 secondary pocket. Thus, we expect the compounds show good potency and selectivity on COX-2 inhibition.

Keywords

• Azido Pharmacophore
• COX-2 inhibitors
• Hydrazide Moiety

Main Subjects

• Medicinal chemistry

---